Prodilidine
Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain.
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- CAS No.: 3734-17-6
- Formule: C15H21NO2
- Masse moléculaire:247.34
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Prodilidine undergoes N-demethylation via liver microsomes from multiple species, with the (-)-Prodilidine showing greater demethylation than the (+)-Prodilidine by rat liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Prodilidine hydrochloride (11.2-17.8 mg/kg; p.o.; s.c.; i.v.) exhibits analgesic activity in rats, with ED50 values ranging from 11.2 mg/kg (intravenous) to 17.3 mg/kg (oral) in the tail-flick assay, and LD50 values ranging from 74 mg/kg (intravenous) to 253 mg/kg (oral)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:84.0 mg/kg (tail-pinch assay, p.o.); 72.3 mg/kg (tail-pinch assay, s.c.); 30.0 mg/kg (tail-pinch assay, i.v.); 7.2 mg/kg (writhing assay, s.c.); 318 mg/kg (LD50, p.o.); 194 mg/kg (LD50, s.c.); 91 mg/kg (LD50, i.v.)
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Administration:p.o. (tail-pinch assay); s.c. (tail-pinch assay, writhing assay); i.v. (tail-pinch assay)
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Result:Achieved an ED50 of 84.0 mg/kg orally in the tail-pinch assay.
Achieved an ED50 of 72.3 mg/kg subcutaneously in the tail-pinch assay.
Achieved an ED50 of 30.0 mg/kg intravenously in the tail-pinch assay.
Achieved an ED50 of 7.2 mg/kg subcutaneously in the writhing assay.
Reached an LD50 of 318 mg/kg orally in mice.
Reached an LD50 of 194 mg/kg subcutaneously in mice.
Reached an LD50 of 91 mg/kg intravenously in mice.
Chemical Information
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CAS No. 3734-17-6
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Masse moléculaire 247.34
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Formule C15H21NO2
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SMILES
O=C(OC1(C=2C=CC=CC2)CCN(C)C1C)CC
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Synonyms
CI-427
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Prodilidine Related Classifications
HY-105628 Related Classifications
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